A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 47/48 (2006.01) C07K 14/76 (2006.01) C07K 14/79 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2265861
This invention concerns conjugates of transferrin, albumin and polyethylene glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approx. 5000 and 200 000) with at least one HS- , HO- or H2N group and cytostatic compounds derived through maleinimide or N- hydroxysuccinimide ester-compounds, such as doxorubicene, daunorubicene, epirubicene, idarubicene, mitoxandrone, chlorambucil, melphalan, 5- fluorouracyl, 5'-desoxy-5-fluorouridene, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecene, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbin or a compound of general formula A, B, C or D, where n = 0-6, X = -NH2, -OH, -COOH, -O-CO-R- COR*, -NH-CO-R-COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstitued phenylene group and R* H, phenyl, alkyl with 1-6 carbon atoms.
L'invention concerne des conjugués de transferrine, d'albumine et de polyéthylèneglycol comprenant de la transferrine ou de l'albumine native ou thiolée ou du polyéthylèneglycol (masse moléculaire comprise entre approximativement 5.000 et 200.000), avec au moins un groupe HS, HO ou H¿2?N, et des composés cytostatiques dérivés de composés imide maléique ou N-hydroxysuccinimidester, tels que doxorubicine, daunorubicine, idarubicine, mitoxandron, chlorambucil, melphalan, 5- fluoro-uracil, 5'-désoxy-5-fluoro-uridine, thioguanine, méthotrexat, paclitaxel, docétaxel, toptécan, 9- aminocamptothécine, étoposide, téniposide, mitopodozide, vinblastine, vincristine, vindésine, vinorelbine ou un composé des formules générales A, B, C ou D: formule A, formule B, formule C, formule D, où n vaut entre 0 et 6, X désigne -NH¿2?, -OH, -COOH, -O-CO-R-COR*, -NH-CO-R-COR*, R désignant une chaîne de carbone aliphatique comportant entre 1 et 6 atomes de carbone ou un groupe phénylène substitué ou non substitué et R* désigne H, phényle, alkyle ayant entre 1 et 6 atomes de carbone.
Kratz Felix
Moffat & Co.
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